CAS: 2236-60-4; 2-Aminopteridin-4(8H)-One

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📜2-Amino-3-[2-(4-Nitrophenyl)Ethyl]Pteridin-4(3H)-One置于1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 24.0H,以92%的收率获得2-氨基-4-羟基蝶啶
参考文献:蝶啶,Cxiii部分†
标题:蝶啶,Cxiii部分†
摘要:蝶呤的低溶解度可通过n 2-酰化或形成n 2-[((二甲基氨基)亚甲基]衍生物而大大改善.这两种类型的化合物可以下被烷基化的mitsunobu条件从到形式ñ 2-Acylpterins(参照2和3)和它们的衍生物(参见图5,6,8,9,11,13,15,和17)选择性地将ò 4-烷基衍生物22-31,而给电子体[[(二甲基氨基)亚甲基氨基]在46-51在选择性反应中给出n(3)取代(52-61).ñ 2,ñ 2个-Dimethylpterins和18个19和ñ 2-Methylpterins 20和21直接烷基化还向ò 4位上(32-35,38和39).脱酰可以在非常温和的条件下通过溶剂解用meoh(实现22 40,26 41),和所述的位移ò 4-[2-(4-硝基苯基)乙基]基团在室温下,以相应的蝶啶-2,4-二胺氨前进42-45.N 2-[((二甲基氨基)亚甲基]基团的裂解可很好地与氨(62
Doi:10.1002/hlca.200390025

专利信息

专利号:US-2004053355-A1
优先权日:2000-05-26
标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors
发明人：WAINER IRVING; MARKOGLOU NEKTARIA
摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.

专利号:US-6319905-B1
优先权日:1998-12-29
标 题 :Method of controlling L-Dopa production and of treating dopamine deficiency
发明人：MANDEL RONALD J; LEFF STUART E
权利人:CELL GENESYS INC
摘要:The present invention provides an effective approach to achieve the tightly modulated production of L-DOPA and/or dopamine at a preselected target location in the brain of a mammal by combining gene therapy approaches to supply a key enzyme in the synthesis of L-DOPA, and novel drug delivery modalities to administer a uniform level of a modulator of the activity of such key enzyme. The fine-tuned administration of the modulator establishes continuously uniform levels of modulator which in turn allow the effective modulation of L-DOPA and/or dopamine levels at a preselected target location in the brain of the mammal.

专利号:WO-2018165051-A1
优先权日:2017-03-06
标 题 :Apparatus, methods, and medicaments for treatment of insect pollinators
发明人：BUTZLOFF PETER ROBERT
权利人:BUTZLOFF PETER ROBERT
摘要:An insect pollinator compartment having a wall transparent to therapeutic light frequency delivered to an insect pollinator in an interior of the compartment. Bee hive includes top box, bottom box, and middle hive box. Top box light is a green color, bottom box light is red or infrared color, and middle box light is a yellow or orange color. An artificial photosensitizer, fulierol-8 [C60(OH)8] effects photolysis in the bees in the presence of a therapeutic light. Data acquisition module coupled to a hive scale beneath the bee hive; a C02 sensor in the bottom box; a relative humidity sensor; a light sensor module sensing internal and external luminosity; a temperature sensor sensing internal and external temperatures; a sound sensor; a communication module; a computer and a power module. Methods provide for synthesis of fullerol-8, and for preparation of fullerol-8 medicament.

专利号:US-9574189-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries
发明人：FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).

专利号:US-11718864-B2
优先权日:2015-09-23
标 题 :Cells and method of cell culture
发明人：HILLER GREGORY WALTER; MITCHELL JEFFREY JOSEPH; MULUKUTLA BHANU CHANDRA; PEGMAN PAMELA MARY
权利人:PFIZER
摘要:The invention relates to a method of cell culture where the cells are modified to reduce the level of synthesis of growth and/or productivity inhibitors by the cell. The invention also relates to a method of cell culture for improving cell growth and productivity, in particular in fed-batch culture of mammalian cells at high cell density. The invention further relates to a method of producing cells with improved cell growth and/or productivity in cell culture and to cells obtained or obtainable by such methods.

专利号:US-5401844-A
优先权日:1983-04-11
标 题 :Regulation of enzymes which utilize tetrahydrobiopterin or tetrahydrofolate cofactors with 6,6-disubstituted-tetrahydropteridines
发明人：AYLING JUNE E; BAILEY STEVEN W
权利人:UNIV SOUTH ALABAMA
摘要:6-[2'-Amino-2',2'-disubstituted-ethylamino]-pyrimidines of the structure: ##STR1## in which X=H, NH 2 or NO 2 , which are novel intermediates in the synthesis of quinoid 6,6-disubstituted-dihydro- and 6,6-disubstituted-tetrahydro-pteridines, are claimed.